Drug intelligence / Profile preview

trilaciclib + sacituzumab tirumotecan

Development stage
Preclinical
Lead developer
Kelun-Biotech
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

**Trilaciclib + sacituzumab tirumotecan** is an experimental combination regimen comprising two agents: *trilaciclib*, an intravenous CDK4/6 inhibitor designed for myeloprotection, and *sacituzumab tirumotecan*, an antibody-drug conjugate targeting TROP2 and delivering a belotecan-derived topoisomerase I inhibitor. Trilaciclib is administered to preserve hematopoietic stem and progenitor cells and reduce chemotherapy-induced myelosuppression when given before cytotoxic agents. Sacituzumab tirumotecan targets TROP2-expressing tumor cells, facilitating internalization and release of its cytotoxic payload, leading to DNA damage and cell death. The rationale for combining these agents is to decrease the risk of hematological adverse events and potentially improve the tolerability of treatment, particularly in patients with unresectable locally advanced or metastatic solid tumors, such as triple-negative breast cancer (TNBC)[5][3]. Clinical investigation of this combination, as of 2025, remains in early stages, primarily in phase 1/2 safety and efficacy studies in advanced solid tumors.

Brand names
trilaciclib: Coselasacituzumab tirumotecan: Jiataile
Other names
none specific for the combination
02

Targets

TOP1 (DNA Topoisomerase I)CDK6 (Cyclin-dependent kinase 6)TACSTD2 (Tumor-associated calcium signal transducer 2)CDK4 (Cyclin-dependent kinase 4)

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